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Edicotinib

Edicotinib
Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
Catalog No. T15199Cas No. 1142363-52-7
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Purity:99.69%
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Edicotinib

Catalog No. T15199Cas No. 1142363-52-7
Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
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Pack SizePriceAvailabilityQuantity
1 mg$64In Stock
2 mg$93In Stock
5 mg$155In Stock
10 mg$228In Stock
25 mg$397In Stock
50 mg$583In Stock
100 mg$813In Stock
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Product Introduction

Bioactivity
Description
Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
Targets&IC50
FLT3:190 nM, c-Kit:20 nM , CSF1R:3.2 nM
In vitro
Edicotinib (0.1 nM-1μM; 24 hours) causes a dose-dependent decrease of CSF1R activation. Edicotinib (0.1 nM-1μM; 24 hours) lead to a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose-response curve displays the effect of Edicotinib on CSF1R and ERK1/2 (IC50: 18.6 nM and 22.5 nM for CSF1R and ERK1/2) [1].
In vivo
Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced, however not other inflammatory cytokines. Edicotinib (oral gavage; 3, 10, 30, and 100 mg/kg; 5 days) obviously inhibits microglial proliferation in ME7 mice.?It reduces the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg. At every dose tested (CD45+CD11b high Ly6C intermediate/low cells), JNJ-527 depletes up to 50% of patrolling blood monocytes. Only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high?cells) at 100 mg/kg [1]. Edicotinib displays a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively [1].
AliasJNJ-527, JNJ-40346527
Chemical Properties
Molecular Weight461.6
FormulaC27H35N5O2
Cas No.1142363-52-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 1 mg/mL, Sonication is recommended.

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